N-(6-CHLORO-9H-PYRIDO[3,4-B]INDOL-8-YL)-3-PYRIDINECARBOXAMIDE DIHYDROCHLORIDE

Product Name: N-(6-CHLORO-9H-PYRIDO[3,4-B]INDOL-8-YL)-3-PYRIDINECARBOXAMIDE DIHYDROCHLORIDE
CAS No.: 431898-65-6
Chemical Name: N-(6-CHLORO-9H-PYRIDO[3,4-B]INDOL-8-YL)-3-PYRIDINECARBOXAMIDE DIHYDROCHLORIDE
Synonyms: PS 1145;CS-2600;PS 1145;PS1145;IKK Inhibitor X;PS-1145 DIHYDROCHLORIDE;N-(6-chloro-9H-pyrido[3,4-b]indol-8-yl)pyridine-3-carboxamide;3-Pyridinecarboxamide, N-(6-chloro-9H-pyrido[3,4-b]indol-8-yl)-;N-(6-CHLORO-9H-PYRIDO[3,4-B]INDOL-8-YL)-3-PYRIDINECARBOXAMIDE DIHYDROCHLORIDE
CBNumber: CB9831263
Molecular Formula: C17H11ClN4O
Formula Weight: 322.75
MOL File: 431898-65-6.mol

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N-(6-CHLORO-9H-PYRIDO[3,4-B]INDOL-8-YL)-3-PYRIDINECARBOXAMIDE DIHYDROCHLORIDE Property

Boiling point:: 511.0±50.0 °C(Predicted)
Density: 1.513±0.06 g/cm3(Predicted)
storage temp.: 2-8°C
solubility: DMSO: >3mg/mL at ~60°C, clear (with warming for 2 minutes)
pka: 11.75±0.43(Predicted)
form: solid
color: yellow

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Safety

Hazard Codes: Xn
Risk Statements: 22
WGK Germany: 3

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

Precautionary statements

P280Wear protective gloves/protective clothing/eye protection/face protection.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: P6624
Product name: PS-1145 dihydrochloride
Purity: ≥98% (HPLC), solid
Packaging: 5mg
Price: $85.6
Updated: 2024/03/01

Sigma-Aldrich

Product number: P6624
Product name: PS-1145 dihydrochloride
Purity: ≥98% (HPLC), solid
Packaging: 25mg
Price: $684
Updated: 2024/03/01

Cayman Chemical

Product number: 14862
Product name: PS-1145
Purity: ≥98%
Packaging: 500μg
Price: $32
Updated: 2024/03/01

Cayman Chemical

Product number: 14862
Product name: PS-1145
Purity: ≥98%
Packaging: 1mg
Price: $50
Updated: 2024/03/01

Cayman Chemical

Product number: 14862
Product name: PS-1145
Purity: ≥98%
Packaging: 5mg
Price: $130
Updated: 2024/03/01

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N-(6-CHLORO-9H-PYRIDO[3,4-B]INDOL-8-YL)-3-PYRIDINECARBOXAMIDE DIHYDROCHLORIDE Chemical Properties,Usage,Production

Uses

N-(6-Chloro-9H-pyrido[3,4-b]indol-8-yl)-3-pyridinecarboxamide is an inhibitor of IKKβ, an enzyme involved with the cytokine-activated intracellular signaling pathway that regulates the immune response. N-(6-Chloro-9H-pyrido[3,4-b]indol-8-yl)-3-pyridinecarboxamide also inhibits osteoclast differentiation.

Uses

PS-1145 dihydrochloride has been used as an IκB kinase (IKK) inhibitor:

in the culture medium to treat human epidermal keratinocytes (HEKs) and squamous carcinoma cells (SCCs) to study the role of IKK in?Corynebacterium tuberculostearicum?(C. t.)-elicited transcription of inflammatory mediators
to investigate the involvement of transcription factor p65 (RelA)/nuclear factor kappa-B (NF-κB) in the cluster of differentiation 28 (CD28)-mediated interleukin-17A (IL-17A) gene expression
to examine the involvement of NF-κB signaling in the cytotoxic effect of niclosamide on colorectal cancer (CRC) cells

Definition

ChEBI: N-(6-chloro-9H-pyrido[3,4-b]indol-8-yl)-3-pyridinecarboxamide is a member of beta-carbolines.

Biological Activity

ps-1145 is an ikappab kinase (ikk) inhibitor.the iκb kinase is an enzyme complex involved in propagating the cellular response to inflammation. this enzyme complex is reported to be part of the upstream nf-κb signal transduction cascade.

Biochem/physiol Actions

PS-1145, a β-carboline derivative, blocks the phosphorylation and degradation of the inhibitor of nuclear factor kappa-β (NF-κB;). It also inhibits the subsequent activation of nuclear factor kappa-β (NF-κB) and thereby prevents the release of tumor necrosis factor-α (TNF-α) in lipopolysaccharide treated mice. PS-1145 hinders pro-inflammatory cytokine production and cell proliferation. It plays a potential therapeutic role in carcinogenesis in multiple myeloma. PS-1145 exhibits anti-tumor activity on nasopharyngeal carcinoma (NPC) cell lines.

in vitro

previous study found that ps-1145 could block tnfalpha-induced nf-kappab activation in a dose- and time-dependent manner in mm cells, which up-regulated ikappabalpha protein, enhanced blockade of nf-kappab activation. in addition, ps-1145 blocked the protective effect of il-6 against dex-induced apotosis and tnfalpha-induced icam-1 expression was also inhibited by ps-1145. moreover, ps-1145 inhibited both il-6 secretion from bmscs triggered by mm cell adhesion and proliferation of mm cells adherent to bmscs. however, ps-1145 could only partially inhibit mm cell proliferation. importantly, it was found that tnfalpha induced mm cell toxicity in the presence of ps-1145 [1]

in vivo

animal study showed that the intravenous application of ps-1145 could promote direct apoptosis in dmba-induced skin tumor in male wistar rats via blocking nf-κb and vegf activities [2].

IC 50

88 nm

References

[1] hideshima t,chauhan d,richardson p,mitsiades c,mitsiades n,hayashi t,munshi n,dang l,castro a,palombella v,adams j,anderson kc. nf-kappa b as a therapeutic target in multiple myeloma. j biol chem.2002 may 10;277(19):16639-47.
[2] rajmani rs,gandham rk,gupta sk,et al. administration of iκb-kinase inhibitor ps1145 enhances apoptosis in dmba-induced tumor in male wistar rats. cell biol int.2015 nov;39(11):1317-28.

N-(6-CHLORO-9H-PYRIDO[3,4-B]INDOL-8-YL)-3-PYRIDINECARBOXAMIDE DIHYDROCHLORIDE Preparation Products And Raw materials

Raw materials

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N-(6-CHLORO-9H-PYRIDO[3,4-B]INDOL-8-YL)-3-PYRIDINECARBOXAMIDE DIHYDROCHLORIDE Suppliers

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View Lastest Price from N-(6-CHLORO-9H-PYRIDO[3,4-B]INDOL-8-YL)-3-PYRIDINECARBOXAMIDE DIHYDROCHLORIDE manufacturers

Career Henan Chemical Co

Product: N-(6-chloro-9H-pyrido[3,4-b]indol-8-yl)pyridine-3-carboxamide 431898-65-6
Price: US $9.80/KG
Min. Order: 1KG
Purity: ≥98%
Supply Ability: 20 tons
Release date: 2020-01-09

431898-65-6, N-(6-CHLORO-9H-PYRIDO[3,4-B]INDOL-8-YL)-3-PYRIDINECARBOXAMIDE DIHYDROCHLORIDERelated Search:

N-(6-chloro-9H-pyrido[3,4-b]indol-8-yl)pyridine-3-carboxamide

IKK Inhibitor X

PS 1145

N-(6-CHLORO-9H-PYRIDO[3,4-B]INDOL-8-YL)-3-PYRIDINECARBOXAMIDE DIHYDROCHLORIDE

PS-1145 DIHYDROCHLORIDE

PS 1145;PS1145

CS-2600

3-Pyridinecarboxamide, N-(6-chloro-9H-pyrido[3,4-b]indol-8-yl)-

431898-65-6

31898-65-6

C17H11ClN4O2HCl

A cell-permeable β-carboline compound that displays anti-inflammatory properties.